loperamide

Loperamide is a synthetic antidiarrheal medication classified as an opioid receptor agonist, primarily used to control and relieve symptoms of acute and chronic diarrhea, including that associated with inflammatory bowel disease, short bowel syndrome, and irritable bowel syndrome. It is also used to reduce stool output in patients with ileostomies. Loperamide acts by binding to mu-opioid receptors in the gut wall, inhibiting the release of acetylcholine and prostaglandins. This action reduces peristalsis (intestinal motility), increases intestinal transit time, enhances water and electrolyte absorption from the intestines, increases anal sphincter tone (reducing urgency), and results in firmer stools with decreased frequency[2][3][4][5][6][7]. At therapeutic doses it does not cross the blood-brain barrier or produce central opioid effects; however, at high doses or when P-glycoprotein-mediated efflux is inhibited, it may cause central nervous system toxicity. Overdose can result in serious cardiac arrhythmias due to inhibition of sodium channels and potassium channels involved in cardiac conduction[1][4]. Loperamide was first synthesized in 1969 and approved for medical use in 1976.

Brand names

ImodiumImodium A-DDiamodeImogenImotilImperimKaodene A-DKao-Paverin CapsMaalox Anti-DiarrhealPepto Diarrhea Control

Other names

loperamide hydrochloride